Thanks to a new synthetic approach recently developed by us1, a new series of pyrrolo[3,2-c]quinoline (PQ) derivatives, has been synthesized permitting us to introduce suitable functional groups in different positions of the scaffold. The latter known for possessing a wide range of biological activities, including anticancer2. The one dose screening (10 ?M) performed by the National Cancer Institute (NCI, USA) against 60 types of tumor cell lines including several panel such as leukemia, lung, renal, CNS, prostate, breast, melanoma, ovarian and colon cancers, allowed us to identify a clear profile of selectivity and potency. Thus, for the most promising derivatives, we undertaken in dept biological investigations. In detail, the 4-substituted piperonil one, which exhibited a preliminary 58% and 18% of growth inhibition in the NCI testing against MCF-7 and MDA-MB-231, respectively, are here submitted to further investigations in order to get new insights on the mode of action. Therefore, a dose response profile at 24, 48 and 72 h was undertaken. More details will be shown at the poster session
Antiproliferative activity of Pyrrolo[3,2-c]quinoline derivatives against breast cancer cells
F Mingoia;C Di Sano;L Minafra
2016
Abstract
Thanks to a new synthetic approach recently developed by us1, a new series of pyrrolo[3,2-c]quinoline (PQ) derivatives, has been synthesized permitting us to introduce suitable functional groups in different positions of the scaffold. The latter known for possessing a wide range of biological activities, including anticancer2. The one dose screening (10 ?M) performed by the National Cancer Institute (NCI, USA) against 60 types of tumor cell lines including several panel such as leukemia, lung, renal, CNS, prostate, breast, melanoma, ovarian and colon cancers, allowed us to identify a clear profile of selectivity and potency. Thus, for the most promising derivatives, we undertaken in dept biological investigations. In detail, the 4-substituted piperonil one, which exhibited a preliminary 58% and 18% of growth inhibition in the NCI testing against MCF-7 and MDA-MB-231, respectively, are here submitted to further investigations in order to get new insights on the mode of action. Therefore, a dose response profile at 24, 48 and 72 h was undertaken. More details will be shown at the poster sessionI documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.